PEG-functionalized magnetic nanoparticles for drug delivery and magnetic resonance imaging applications.

PEG-functionalized magnetic nanoparticles for drug delivery and magnetic resonance imaging applications.
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DOI:
10.1007/s11095-010-0260-1
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发表时间:
2010-11
影响因子:
3.7
通讯作者:
Labhasetwar, Vinod
Labhasetwar, Vinod
中科院分区:
医学3区
文献类型:
--
作者:
Yallapu, Murali Mohan;Foy, Susan P.;Jain, Tapan K.;Labhasetwar, Vinod

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测试了聚乙二醇化磁性纳米颗粒(MNPs)作为药物载体系统、磁共振成像(MRI)试剂以及与抗体偶联的能力。氧化铁核包覆油酸,然后涂上油酸-聚乙二醇酯,形成可水分散的MNP配方。疏水性多柔比星可进入OA层,实现药物的持续输送。测定小鼠颈动脉T1、T2磁共振成像对比度,并测定MNPs的循环情况。在人乳腺癌细胞系MCF-7中,用聚乙二醇酸-80上的N-羟基琥珀酰亚胺基团(NHS)与抗体偶联,用于主动靶向。最优处方的平均流体力学直径为184 nm,核心为8 nm的氧化铁。MNPs增强T2磁共振对比度,在体内循环时间较长,注射后50min相对浓度为30%。载阿霉素的多柔比星纳米粒在体外具有缓释和剂量依赖性的抗增殖作用,转铁蛋白抗体偶联的多柔比星纳米粒的药物效应增强。聚乙二醇化的MNPs可作为靶向给药系统和MRI造影剂。
Polyethylene glycol (PEG) functionalized magnetic nanoparticles (MNPs) were tested as a drug carrier system, magnetic resonance imaging (MRI) agent, and ability to conjugate to an antibody. An iron oxide core coated with oleic acid (OA) and then with OA-PEG forms a water dispersible MNP formulation. Hydrophobic doxorubicin partitions into the OA layer for sustained drug delivery. The T1 and T2 MRI contrast properties were determined in vitro and the circulation of the MNPs measured in mouse carotid arteries. An N-hydroxysuccinimide group (NHS) on the OA-PEG-80 was used to conjugate the amine functional group on antibodies for active targeting in the human MCF-7 breast cancer cell line. The optimized formulation had a mean hydrodynamic diameter of 184 nm with an 8 nm iron-oxide core. The MNPs enhance the T2 MRI contrast, and have a long circulation time in vivo with 30% relative concentration 50 min post-injection. Doxorubicin-loaded MNPs showed sustained drug release and dose-dependent antiproliferative effects in vitro; the drug effect was enhanced with transferrin antibody conjugated MNPs. PEG functionalized MNPs could be developed as a targeted drug delivery system and MRI contrast agent.
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